Sunitinib Malate

Licensed by Pfizer Catalog No.S1042

Sunitinib Malate Chemical Structure

Molecular Weight(MW): 532.56

Sunitinib Malate is a multi-targeted RTK inhibitor targeting VEGFR2 (Flk-1) and PDGFRβ with IC50 of 80 nM and 2 nM in cell-free assays, and also inhibits c-Kit.

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In DMSO USD 191 In stock
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USD 147 In stock
USD 447 In stock
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Cited by 42 Publications

12 Customer Reviews

  • PDGF-AA induces Ezh2 expression and proliferation in juvenile islets but not in adult islets. Western immunoblots of indicated islet proteins from 3 week or 9 month-old WT islets 2 days after exposure to PDGF-AA alone, or PDGF-AA plus RTK inhibitors Sunitinib.

    Nature 2011 478(7369):349-55. Sunitinib Malate purchased from Selleck.

    Assessment of effects on human juvenile or adult islets after exposure to PDGF-AA (50 ng/ml) for 2 days, with or without Sunitinib (2 uM) or U0126 (10 uM)co-treatment. Average percentage of BrdU+ insulin+ cells was morphometry from sectioned islets immunostained for insulin (green), glucagon (white) and BrdU (red). n = 3-6 independent experiments.

    Nature 2011 478(7369):349-55. Sunitinib Malate purchased from Selleck.

  • Combinational treatment of kinase inhibitors induces the similar phenotype produced by PP1. All images are lateral view with dorsal to the top and anterior to the left. The combinational treatment of Dasatinib (D) or U0126 (U) with Sunitinib (SU),PTK787 (PTK), or ZM323881 (Z) resulted in the shrinkage of dorsal aorta.

    Cell Res 2011 21, 1080-1087. Sunitinib Malate purchased from Selleck.

    A, Tumor growth curves from the initial sunitinib drug trials, with endpoint set at 1,300 mm3 (mean ± SEM). Measurements began one week after tumor inoculation and on the day sunitinib treatment began. Subsequent experimental endpoints were set on the basis of these growth curves and their intersections with this data are shown. B, Histogram plot showing the distribution of tumor sizes at day 8 of treatment. Sunitinib-treated tumors exceeding 250 mm3 in size were identified as falling into the nonresponsive cohort. Sunitinib treatment significantly retards growth of responsive tumors.

    Cancer Res, 2017, 77(4):1008-1020 . Sunitinib Malate purchased from Selleck.

  • Sunitinib decreases FLT-3 and RET phosphor ylation but increases ERK phosphorylation in a time-dependent manner. H295R and SW13 cells were treated with sunitinib (10 nM) for various time points as indi-cated. Cell lysates were prepared and phospho-FLT-3, RET, and ERK levels were monitored by Western Blot-ting. Re-probing against FLT-3, RET, and ERK was done to ensure equal protein loading.

    Surgery 2012 152, 1045-50. Sunitinib Malate purchased from Selleck.

    Sunitinib or PD98059 decreases cell proliferation in a dose-dependent manner. H295R and SW13 cells were treated with various concentration of sunitinib or PD98059 for 48 hours as indicated. Treated cells were subjected to the MTS proliferation assay. Similar experiments were repeated 3 times. Histograms represent relative % of OD490 nm absorbance (* P < .05). All data are relative multiples of expression compared with untreated cells. The data are representative of three experiments and are expressed as the mean ?SE.

    Surgery 2012 152, 1045-50. Sunitinib Malate purchased from Selleck.

  • Autophagic activation in sunitinib- and sorafenib- but not AZD6244-treated cells. Medullary thyroid cancer-1.1 (MTC-1.1; A) and TT ( B) cells were treated with dimethyl sulfoxide (DMSO), sunitinib (50 nM), sorafenib (10 nM), AZD6244 (30 nM), or everolimus (20 nM) for 48 hours. Cell lysates were prepared, and light chain 3 (LC3)-I and -II cleaved caspase-3 protein levels were monitored by Western blotting. Reprobing against actin was per formed to ensure equal protein loading. ( C ) MTC-1.1 and TT cells were transiently transfected with autophagy protein 5 (Atg-5) small inter fering RNA. Transfection with scrambled small inter fering RNA was used as a control. After transfection, cells with and without Atg-5 knockdown were exposed to DMSO or 20 nM of everolimus for 48 hours. Cell lysates were pre- pared and LC3-I and -II protein expression levels were monitored by Western blotting. Reprobing against Atg-5 was per formed to monitor Atg-5 knockdown efficiency. Reprobing against actin was per formed to ensure equal protein.

    Surgery 2012 152, 1142-9. Sunitinib Malate purchased from Selleck.

    Autophagy inhibition blocks the antiproliferative effects of sunitinib and sorafenib but not AZD6244. Medullary thyroid cancer–1.1 (MTC-1.1) and TT cells were transfected transiently with scrambled or autophagy protein 5 (Atg-5) small inter fering RNA. After transfection, cells with and without Atg-5 knockdown were exposed to sunitinib (50 nM), sorafenib (10 nM), and AZD6244 (30 nM) for 48 hours. Treated cells were subjected to a 3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2H-tetrazolium proliferation assay. Similar experiments were repeated 3 times. Histograms represent the relative percent of OD490 nM absorbance. The asterisk indicates significance versus scrambled small inter fering RNA–treated control ( P < .05). All data are relative multiples of expression compared to untreated cells. The data are representative of 3 experiments and are expressed as the mean ± the standard error.

    Surgery 2012 152, 1142-9. Sunitinib Malate purchased from Selleck.

  • Sunitinib limits the colonial growth of HT-29 by downregulating HIF-1a. (A) The number and size of colonies formed in soft agar. The numbers of small colonies (<50 μm diameter) were not different among conditions of a serial concentration of sunitinib. On the contrary, large colonies (>50 μm diameter) disappeared after incubation with sunitinib. Each point represents the mean and SD from four separate experiments. (B) HIF-1a expression and hypoxia within HT-29 colony. After colonies grew for 4 weeks, HIF-1a and hypoxia were visualized by immunofluoroscence staining. Bar = 20 μm.

    Biochem Bioph Res Co 2010 398, 205–211. Sunitinib Malate purchased from Selleck.

    2. Sunitinib downregulates HIF-1a. (A) Dose-dependent repression of HIF-1a protein level by sunitinib in HT-29. HT-29 cells were incubated under normoxic (N) or hypoxic (H) conditions in the presence of sunitinib for 24 h. HIF-1a and ARNT proteins in total cell lysates were analyzed by Western blotting. (B) Sunitinib attenuates the hypoxic induction of HIF-1 target genes. RNAs were isolated from HT-29 cells subjected to normoxia (N) or hypoxia (H) in the presence of sunitinib for 16 h. The mRNAs of HIF-1a and its target genes were analyzed by RT-PCR and autoradiography. PGK1 indicates phosphoglycerate kinase 1; PDK1, pyruvate dyhydrogenase kinase 1; CAIX, carbonic anhydrase IX. (C) Sunitinib-induced HIF-1 inhibition. Epo-enhancer and b- galactosidase reporter plasmids were co-transfected into HEK293 cells. After 16 h incubation, luciferase and b-galactosidase activities were measured. *P < .05 versus the hypoxic control.

     

     

    Biochem Bioph Res Co 2010 398, 205–211. Sunitinib Malate purchased from Selleck.

  • Sunitinib inhibits 50-UTR-dependent translation of HIF-1a. (A) 50 cap-dependent translational activity of HIF-1a. The luciferase reporter plasmid contains the HIF-1a 50-UTR segment between the tk promoter and the luciferase gene. HT-29 cells were co-transfected with the reporter plasmid (8 lg per 100-mm dish) and the b-gal plasmid (4 μg). After 16 h incubation under normoxic or hypoxic conditions with sunitinib, cells were lysed and subjected to luciferase assay. *P < .05 versus the hypoxic control. (B) IRES-dependent translational activity of HIF-1a. The luciferase reporter plasmid contains the HIF-1a 50-UTR segment between the GFP gene and the luciferase gene. HT-29 cells were co-transfected with the reporter plasmid (8 μg) and the b-gal plasmid (4 μg). *P < .05 versus the hypoxic control. (C) Sunitinib inhibits phosphorylation of Akt. After 8 h incubation under hypoxic condition with sunitinib, HT-29 cells were lysed and subjected to Western blotting. (D) Sunitinib suppresses HIF-1a in VHL-null RCC4 cells. VHL (-/-) RCC4 cells were incubated under normoxic conditions sunitinib for 8 h, and HIF-1a in total cell lysates was analyzed by Western blotting.

     

     

    Biochem Bioph Res Co 2010 398, 205–211. Sunitinib Malate purchased from Selleck.

    Experimental layout for VEGF signaling blocking and LCMV infection in WT mice. Mice received two injections on day 0 and 3 p.i. of Abs as described in Material and Methods, or daily gavage of the VEGFR/PDGFR-inhibitor sunitinib. Inguinal LN volume on day 0 (D0) or day 8 (D8) p.i. after treatment of mice with control Ig or anti-VEGFR2, anti-VEGF-A Abs or sunitinib. Pooled from 1-2 independent experiments with 3-5 mice per treatment. D. Total HEV length on day 0 (D0) or day 8 (D8) p.i. as in C. No significant difference was found in C and D between day 8 control Ig and Ab- or inhibitor-treated values (One-way ANOVA).

    AACR Sunitinib Malate purchased from Selleck.

Purity & Quality Control

Choose Selective PDGFR Inhibitors

Biological Activity

Description Sunitinib Malate is a multi-targeted RTK inhibitor targeting VEGFR2 (Flk-1) and PDGFRβ with IC50 of 80 nM and 2 nM in cell-free assays, and also inhibits c-Kit.
Targets
Kit [1]
(Cell-free assay)
FLT3 [1]
(Cell-free assay)
PDGFRβ [1]
(Cell-free assay)
VEGFR2 [1]
(Cell-free assay)
2 nM 80 nM
In vitro

Sunitinib also potently inhibits Kit and FLT-3. [1] Sunitinib is a potent ATP-competitive inhibitor of VEGFR2 (Flk1) and PDGFRβ with Ki of 9 nM and 8 nM, respectively, displaying >10-fold higher selectivity for VEGFR2 and PDGFR than FGFR-1, EGFR, Cdk2, Met, IGFR-1, Abl, and src. In serum-starved NIH-3T3 cells expressing VEGFR2 or PDGFRβ, Sunitinib inhibits VEGF-dependent VEGFR2 phosphorylation and PDGF-dependent PDGFRβ phosphorylation with IC50 of 10 nM and 10 nM, respectively. Sunitinib inhibits VEGF-induced proliferation of serum-starved HUVECs with IC50 of 40 nM, and inhibits PDGF-induced proliferation of NIH-3T3 cells overexpressing PDGFRβ or PDGFRα with IC50 of 39 nM and 69 nM, respectively. [2] Sunitinib inhibits phosphorylation of wild-type FLT3, FLT3-ITD, and FLT3-Asp835 with IC50 of 250 nM, 50 nM, and 30 nM, respectively. Sunitinib inhibits the proliferation of MV4;11 and OC1-AML5 cells with IC50 of 8 nM and 14 nM, respectively, and induces apoptosis in a dose-dependent manner. [3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
3T3 NV;iUYMyU2mwYYPlJGF{e2G7 MWXJcohq[mm2aX;uJI9nKFCGR1[tbY5lfWOnZDDCdoRWKGmwY3;ydI9z[XSrb36ge4l1cCCLQ{WwJI9nKDBwMEC3JO69VQ>? NE\DVYcyOjZ2NkCxPS=>
3T3 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1TVfmlvcGmkaYTpc44hd2ZiUHzheIVt\XRvZHXybZZm\CCpcn;3eIgh\mGldH;yJIlv\HWlZXSgN3Q{KGOnbHygdJJwdGmoZYLheIlwdiC5aYToJGlEPTBib3[gNE4xOSEQvF2= MoPGNVI3PDZyMUm=
3T3 M2O4bWZ2dmO2aX;uJGF{e2G7 NXX2[lJEUW6qaXLpeIlwdiCxZjDWZZNkfWyjcjDlcoRwfGinbHnhcEBoem:5dHig[oFkfG:{IILlZ4VxfG:{IIfpeIghUUN3MDDv[kAxNjB3IN88US=> NH;yTG8yOjZ2NkCxPS=>
3T3 M4TGSGtqdmG|ZTDBd5NigQ>? NUj1SIhVOjBibXnu NFf2UnJFVVOR NUPscHl4S2WubIXsZZIhcW6qaXLpeIlwdiCxZjDWSWdHKGmwZIXj[YQhcHWvYX6gT2RTKHCqb4PwbI9zgWyjdHnvckB4cXSqIFnDOVAhd2ZiMD6wNlIh|ryP MVWxOlE3OjByOB?=
NIH3T3 NYfsR5NDU2mwYYPlJGF{e2G7 M{Do[VIxKG2rbh?= NIDoVYNFVVOR NVLxRlN7cW6qaXLpeEBpfW2jbjDLSHIhc2mwYYPlJIV5eHKnc4Pl[EB4cXSqIFnDOVAhd2ZiMD6wNVgh|ryP NELRfpUyPjF4MkCwPC=>
A549 NIDzRoZHfW6ldHnvckBCe3OjeR?= NETs[YdFVVOR MVfJcohq[mm2aX;uJI9nKGNvTXX0JIRmeGWwZHXueEBJT0ZvaX7keYNm\CCqdX3hckBCPTR7IHPlcIwhdWmpcnH0bY9vKHerdHigTWM2OCCxZjCyJO69VQ>? MYWxPFQ{PDF2NR?=
DU145 NV\NXZRPTnWwY4Tpc44hSXO|YYm= MYXEUXNQ NHftO49KdmirYnn0bY9vKG:oIHOtUYV1KGSncHXu[IVvfCCKR1[tbY5lfWOnZDDoeY1idiCGVUG0OUBk\WyuIIPjZZR1\XKrbnege4l1cCCLQ{WwJI9nKDFyIN88US=> MVixPFQ{PDF2NR?=
KB3-1 MVnDfZRwfG:6aXOgRZN{[Xl? MWG3NkBp MnzzSG1UVw>? MmnkR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gVE1oeC2wZXfheIl3\SCNQj2zMVEh[2WubIOge4l1cCCLQ{WwJI9nKDJwMzFOwG0> Mmj4NVk{QTd|MkK=
KBV1 NHnDSZdEgXSxdH;4bYMhSXO|YYm= M{P6c|czKGh? M2XSbmROW09? NVvONHl7S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hWC2pbInjc5Bzd3SnaX6t[ZhxemW|c3nu[{BMSlZzIHPlcIx{KHerdHigTWM2OCCxZjC0MlEh|ryP NILVUooyQTN7N{OyNi=>
A375 Mo[zR5l1d3SxeHnjJGF{e2G7 MWK3NkBp MYXEUXNQ MlXpTWM2OD13LkSg{txO NHLoU4oyQTZ3NESwPC=>
RS4-11 MkG4SpVv[3Srb36gRZN{[Xl? NI[5VYYzKGh? M{f6d2lvcGmkaYTpc44hd2ZiRlzUN{BifXSxcHjvd5Bpd3K7bHH0bY9vKHerdHigTWM2OCCxZjCwMlAxQTlizszN NIC0fokyQTZ3NESwPC=>
RS4-11 NIfVPGhHfW6ldHnvckBCe3OjeR?= NXX6U2tJOiCq MkCxTY5pcWKrdHnvckBw\iCITGSzJGlVTCCvdYThcpQh[XW2b4Doc5NxcG:{eXzheIlwdiC5aYToJGlEPTBib3[gNE4xOzRizszN MknvNVk3PTR2MEi=
Sf9 M3;WVWtqdmG|ZTDBd5NigQ>? NV\0SFdpOzBibXnu NUPtRWRnUW6qaXLpeIlwdiCxZjDHV3QufGGpZ3XkJHZGT0[UIHX4dJJme3OnZDD3bZRpKEmFNUCgc4YhOC5zOEWg{txO NVXSTIY6OTl6NUSwOVE>
Ba/F3 NGL2b5pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnXNO|IhcA>? MkLCTWM2OD1zLkKg{txO MYSyNFEyPzByNB?=
BaPTC2 NUPiTphYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV23NkBp NV7t[5ZTUUN3ME2wMlIzKM7:TR?= M120VFIxOTF5MEC0
Sf9 MXPGeY5kfGmxbjDBd5NigQ>? M3H3dVEhcA>? NVXwVpRCTE2VTx?= MnLqTY5pcWKrdHnvckBw\iCqdX3hckBz\WOxbXLpcoFvfCCKaYOteIFo\2WmIGLFWEBmgHC{ZYPz[YQhf2m2aDDJR|UxKG:oIEGuN{DPxE1? MViyNFEyPzByNB?=
H4 M4XkbmN6fG:2b4jpZ{BCe3OjeR?= MnrxNVAh|ryP M1rhWnRwgGmlaYT5JIlvKGi3bXHuJGg1KGOnbHzz NXnHXXVSOjB|NUC4NFY>
SF-539 NV3yd21OU2mwYYPlJGF{e2G7 NIL5WFY{OzNizszN Mof6OlAhdWmw NFnMWXFFVVOR MVTJcohq[mm2aX;uJI9nKFCGR1\SZoV1[SCyaH;zdIhwenmuYYTpc44hf2m2aDDJR|UxKG:oIEGyMlIh|ryP MoTSNlA1ODN5MEC=
U251 NHrHOJNMcW6jc3WgRZN{[Xl? NGDmfoQ{OzNizszN MmTrOlAhdWmw M1foNGROW09? MkXlTY5pcWKrdHnvckBw\iCYRVfGVlIheGixc4Doc5J6dGG2aX;uJJdqfGhiSVO1NEBw\iBzOD65JO69VQ>? MWCyNFQxOzdyMB?=
A431 MVjLbY5ie2ViQYPzZZk> NIPWV2FKdmirYnn0bY9vKG:oIGDES2ZT[mW2YTDlfJBz\XO|ZXSge4l1cCCLQ{WwJI9nKDF{LkKg{txO NVP2ZXQyOjB3NUiwO|I>
A431 MmjsT4lv[XOnIFHzd4F6 MnjkTY5pcWKrdHnvckBw\iCYRVfGVlIh\XiycnXzd4VlKHerdHigTWM2OCCxZjCxPE46KM7:TR?= M3LCd|IxPTV6MEey
HepG2 NHm3VYhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4TlOFczKGh? M{TURmlEPTB;Mz64NUDPxE1? MX[yNFU4ODV{Nh?=
Kasumi-1 NUjhVZlYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFzrW2o4OiCq MV;JR|UxRTBwMEG2JO69VQ>? NGfUVFgzODV5MEWyOi=>
RS4-11 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3jaeVczKGh? MmfkTWM2OD1zIN88US=> M33iUVIxPTdyNUK2
THP1 NX\aOHV4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2naUVczKGh? NGLrZlBKSzVyPUCuOUDPxE1? NH[0R20zODV5MEWyOi=>
Kasumi-1 Mlv2SpVv[3Srb36gRZN{[Xl? M{LRd2lvcGmkaYTpc44hd2ZiYz3LbZQh[XW2b4Doc5NxcG:{eXzheIlwdiC5aYToJGlEPTBib3[gNE4xOTVizszN M2TWPFIxQDN|MEO5
A549 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn75NVYhcA>? MUXBcpRqfHWvb4KgZYN1cX[rdImgZYdicW6|dDDoeY1idiCDNUS5JINmdGy| MX:yNVQ2ODR4Mx?=
HL60 Mk\aS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUPLN2RmOTZiaB?= NVfmNnhVSW62aYT1cY9zKGGldHn2bZR6KGGpYXnud5QhcHWvYX6gTGw3OCClZXzsdy=> MV6yNVQ2ODR4Mx?=
HUVEC NVrnN5F3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUWzVXZFOTZiaB?= Mn\0TY5pcWKrdHnvckBw\iCYRVfGMYlv\HWlZXSgZ4VtdCCycn;sbYZmemG2aX;uJJdqfGhiSVO1NEBw\iB{Lke1JO69VQ>? MXqyNVQ2ODR4Mx?=
HUVEC M1r3OGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFfodVUyPiCq NWjn[W94UW6qaXLpeIlwdiCxZjDiSmdHNWmwZIXj[YQh[2WubDDwdo9tcW[ncnH0bY9vKHerdHigTWM2OCCxZjC0MlA1KM7:TR?= M17BZVIyPDVyNE[z
IM9 NWHsNI1wT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4fwWlE3KGh? MmTGRY51cXS3bX;yJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSV25JINmdGy| MoPKNlE1PTB2NkO=
K562 NV:we|NnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{HYXVE3KGh? NXPrS25GSW62aYT1cY9zKGGldHn2bZR6KGGpYXnud5QhcHWvYX6gT|U3OiClZXzsdy=> M1XXdFIyPDVyNE[z
MDA-MB-231 NXm1PZp3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH;R[3IyPiCq MXXBcpRqfHWvb4KgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPRFGtUWIuOjNzIHPlcIx{ MXyyNVQ2ODR4Mx?=
H460 M1TuSGN6fG:2b4jpZ{BCe3OjeR?= MV63NkBp NXnqVoJMUUN3ME2yMlch|ryP MoLQNlE3OjF6OEC=
SMMC7721 NXWzO2hrS3m2b4TvfIlkKEG|c3H5 NF\Fd3g4OiCq NWj6W4xyUUN3ME22MlQ4KM7:TR?= MkTwNlE3OjF6OEC=
WI38 M2DZfmN6fG:2b4jpZ{BCe3OjeR?= M360NVczKGh? M2ezXmlEPTB;OD61OkDPxE1? NHW4PW8zOTZ{MUi4NC=>
HEK293 MXvLbY5ie2ViQYPzZZk> M{DoWFExOCCwTR?= NF6xdmMyKGh? M3r5TIRw\XNibn;0JIlvcGmkaYSgWmVITi2rbnT1Z4VlKGG3dH;wbI9{eGixconsZZRqd25ib3[geJlzd3OrbnWgNVE4PSC{ZYPp[JVmKG:wIG\FS2ZTOiCneIDy[ZN{\WRiaX6gTGVMOjl|IHPlcIx{ MoflNlE5QDV{OEe=
HUVEC MmTySpVv[3Srb36gRZN{[Xl? NXG0SXZnOSEQvF2= NGmxRXIzPCCq MYXBcpRq[W6paX;n[Y5q[yCjY4Tpeol1gSCjc4Pld5Nm\CCjczDk[YNz\WG|ZTDpckBXTUeILXnu[JVk\WRiY3XscEBucWe{YYTpc44> NX33VGNpOjF7NkOzNFU>
HUVEC MYTGeY5kfGmxbjDBd5NigQ>? M1LJcVEh|ryP MX2xJIg> NYPWc2tZUW6qaXLpeIlwdiCxZjDFVmsheGixc4Doc5J6dGG2aX;uJIF1KFSqckKwNk9VgXJ{MESgbY4hXkWJRj3zeIlufWyjdHXkJGhWXkWF Ml7tNlE6PjN|MEW=
HUVEC MYrGeY5kfGmxbjDBd5NigQ>? MXuxJO69VQ>? NWHFe5MxOSCq M{nQSGlvcGmkaYTpc44hd2ZiZV7PV{BxcG:|cHjvdplt[XSrb36gZZQhW2W{LUGxO|IhcW5iVlXHSk1{fGmvdXzheIVlKEiXVlXD MlvQNlE6PjN|MEW=
HUVEC NEi3[lZMcW6jc3WgRZN{[Xl? M{DlPFEh|ryP MlPvNUBp NUT6eZB7UW6qaXLpeIlwdiCxZjDWSWdHWjJicHjvd5Bpd3K7bHH0bY9vKGG2IIT5dk0yOTd3IHnuJHZGT0Zvc4TpcZVt[XSnZDDIWXZGSw>? MlnsNlE6PjN|MEW=
HUVEC Ml\JSpVv[3Srb36gRZN{[Xl? NGHscGgyKM7:TR?= MUGxJIg> MVLkc4V{KG6xdDDpcohq[mm2IFHLWEBxcG:|cHjvdplt[XSrb36gZZQhW2W{LUS3N{BqdiCYRVfGMZN1cW23bHH0[YQhUFWYRVO= MXyyNVk3OzNyNR?=
HL60 NWPQZ|BtS3m2b4TvfIlkKEG|c3H5 MUK1NEDPxE1? MXu0PEBp MUjEUXNQ M{TU[2lEPTB;MUWuOUDPxE1? MoS3NlIxOTlzOEi=
K562 NILQXGxEgXSxdH;4bYMhSXO|YYm= MWG1NEDPxE1? NELmPXg1QCCq Ml;6SG1UVw>? MoHiTWM2OD1{MT65JO69VQ>? NYP3XHdtOjJyMUmxPFg>
PC3 MV7DfZRwfG:6aXOgRZN{[Xl? MoPyOVAh|ryP NVSyU3E2PDhiaB?= M4Tzb2ROW09? NWHKSXFLUUN3ME2yOU4yKM7:TR?= M{GzdVIzODF7MUi4
SF-539 NIHKPI5McW6jc3WgRZN{[Xl? NYHwTIhkOzN|IN88US=> MUe2NEBucW5? Mnv3TY5pcWKrdHnvckBw\iCSRFfGVoJmfGFidInyc5NqdmVia3nuZZNmKGGldHn2bZR6KGmwIGDES2YuSkJvc4TpcZVt[XSnZDDoeY1idiCVRj21N|kh[2WubIOge4l1cCCLQ{WwJI9nKDF{LkKg{txO NVj3eXhCOjJ{MES3OFE>
HAEC NEPSTZlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVuxNFAh|ryP MkjBO|IhcA>? MUjBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEiDRVOgZ4VtdHNiZYjwdoV{e2mwZzDWSWdHWiC5aYToJGlEPTBib3[gNE4yKM7:TR?= MoS1NlI1PDR4N{m=
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MV4-11 M1TFWGN6fG:2b4jpZ{BCe3OjeR?= NYrwZ5FFPzJiaB?= MW\JR|UxRTBwMECzJO69VQ>? Mnz5NlI1PTJ3MUi=
HepG2 NEH2e3NEgXSxdH;4bYMhSXO|YYm= NFK3fYw1QCCq MVHJR|UxRTF|LkK0JO69VQ>? M{ewOlIzPDh|NkC4
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HAEC M{[4bmN6fG:2b4jpZ{BCe3OjeR?= M33lTVExOCEQvF2= NUC2UnFKPzJiaB?= M1LpUGROW09? M33zdWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KF[HR1\SJIV5eHKnc4PpcochUEGHQzD3bZRpKEmFNUCgc4YhOC5zIN88US=> NHzrTI4zOzF|MUW0NS=>
HT-29 MlHnR5l1d3SxeHnjJGF{e2G7 NXvidm53OTByIN88US=> MnvUO|IhcA>? MnuySG1UVw>? NFLGTWxEgXSxdH;4bYNqfHliYXfhbY5{fCCYRVfGVkBmgHC{ZYPzbY5oKGi3bXHuJGhVNTJ7IHPlcIx{KHerdHigTWM2OCCxZjCwMlM{KM7:TR?= M2PnelI{OTNzNUSx
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HUVEC MXzGeY5kfGmxbjDBd5NigQ>? MnHxNkDPxE1? NYTDXWNFOThiaB?= M4fCNGROW09? MlnhRY51cWGwZ3nv[4VvcWNiYXP0bZZqfHliaX6gTHVXTUO|IIXu[IVzKGi7cH;4bYMh[2:wZHn0bY9vKGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4YhfHWkZTDmc5Ju[XSrb36= MVGyN|E2OzJyMB?=
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A498 Ml;YR5l1d3SxeHnjJGF{e2G7 NU[yXYpWOTByIN88US=> M3i2[VczKGh? MYTEUXNQ NHP6RlNKSzVyPUSuN{DPxE1? NYrYRYMyOjN2OEm2NlY>
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A549 MUfDfZRwfG:6aXOgRZN{[Xl? NFzyeFY4OiCq NETEOXVFVVOR MmnkTWM2OD1{LkS0JO69VQ>? MXWyN|YxOjR2MR?=
HCT116 MV7DfZRwfG:6aXOgRZN{[Xl? NHjOO2U4OiCq NXz1d3p5TE2VTx?= MYPJR|UxRTRwN{Gg{txO NE\EfY8zOzZyMkS0NS=>
MCF7 MWTDfZRwfG:6aXOgRZN{[Xl? M4\5SlczKGh? M3LibWROW09? NH65fG5KSzVyPU[uNlkh|ryP MYCyN|YxOjR2MR?=
BGC M3jQSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1vhSVczKGh? M2\ETGROW09? MmHRTWM2OD12Lke4JO69VQ>? MXOyN|k6QTB2MB?=
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HT-29 NFrMfFNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYHmOINbPzJiaB?= NFLjZ3dFVVOR NVf2VnJiUUN3ME2xMlQ4KM7:TR?= NWf0eIlNOjN7OUmwOFA>
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MCF7 NGDvfW9EgXSxdH;4bYMhSXO|YYm= MVe3NkBp NIC4eI9FVVOR NH;rdnRKSzVyPUCuNFI6OyEQvF2= NGHVbIczPDh7ME[1Ni=>
MDA-MB-231 NFf1NnpEgXSxdH;4bYMhSXO|YYm= NVzVRpJJPzJiaB?= NYf1cmJ4TE2VTx?= NF\V[ZZKSzVyPUCuNFIzOyEQvF2= M2XxTFI1QDlyNkWy
MDA-MB-435 NVvmcVVRS3m2b4TvfIlkKEG|c3H5 NYXuW4pNPzJiaB?= NUniRZVVTE2VTx?= MUjJR|UxRTBwMEC5O{DPxE1? MonuNlQ5QTB4NUK=
MDA-MB-468 NGe4enVEgXSxdH;4bYMhSXO|YYm= NEXkdpM4OiCq MWfEUXNQ NUHpNJRmUUN3ME2wMlAxPjFizszN MY[yOFg6ODZ3Mh?=
A431 M{nXOGtqdmG|ZTDBd5NigQ>? MWCxNEDPxE1? MlflNUBp M{LBSmROW09? NFjOZXJKdmirYnn0bY9vKG:oIFXHSnIhf2m2aDDJR|UxKG:oIECuNVczOSEQvF2= MWGyOFg6ODZ3Mh?=
SH-SY5Y MoO0T4lv[XOnIFHzd4F6 NVvTVWhXOTBizszN NYDZUFNNOSCq M33XSGROW09? NVjjRmFZUW6qaXLpeIlwdiCxZjDQSGdHWmKndHGge4l1cCCLQ{WwJI9nKDBwMEizNUDPxE1? NFu2NHIzPDh7ME[1Ni=>
U251 NH\aTZRMcW6jc3WgRZN{[Xl? MmnJNVAh|ryP M4\1UFEhcA>? NWPFWZp1TE2VTx?= MmLNTY5pcWKrdHnvckBw\iCYRVfGVlIhf2m2aDDJR|UxKG:oIECuNFE5QSEQvF2= M3[zRlI1QDlyNkWy
Bel7402 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3TEUVczKGh? MULEUXNQ MVHJR|UxRTJwNkeg{txO M{i2RlI1QTB2OU[x
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MV4-11 MlqyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{jBXVQ5KGh? MXnEUXNQ MlzjTWM2OD1yLkCwN{DPxE1? NXrmUHBGOjR7MES5OlE>
NCI-H3122 NVvYS29PT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX63NkBp NY\CUG9oTE2VTx?= MUTJR|UxRTBwOEOg{txO MluzNlQ6ODR7NkG=
NCI-H460 NHHPPINIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{TJRVczKGh? MoXvSG1UVw>? MmGzTWM2OD12LkOxJO69VQ>? NYXCVIcyOjR7MES5OlE>
NCI-H526 MlvxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVXSV5RGPzJiaB?= NHzFboFFVVOR NYTLem9qUUN3ME2xMlAyKM7:TR?= M4iwVlI1QTB2OU[x
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EoL-1-cell NGjO[5ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGT2[nhKSzVyPUGuOlQheE1? M3;EbXNCVkeHUh?=
MV-4-11 NGmweVRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MofXTWM2OD1{N{KgdG0> MmLPV2FPT0WU
NOS-1 NUnoZ5B{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX3KTY9rUUN3ME2xOU4{KG6P M2XjW3NCVkeHUh?=
CGTH-W-1 NIOxU5lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4nQ[2lEPTB;M{CuPVQhdk1? NFPYT2dUSU6JRWK=
MONO-MAC-6 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2TCcmlEPTB;M{OuPEBvVQ>? MkjkV2FPT0WU
ALL-PO NGPafHRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlW5TWM2OD15OT64PUBvVQ>? NGrDbGVUSU6JRWK=
NKM-1 NUX5VVVjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVnJR|UxRTl6LkWyJI5O MYXTRW5ITVJ?
KM12 M4PZVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH7ZZWVKSzVyPUO1NE4yPCCwTR?= M1OwZnNCVkeHUh?=
TE-15 M4e1Zmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUTLboZwUUN3ME21NFcvPjFibl2= NEnLT4hUSU6JRWK=
697 MnzKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1fRTmlEPTB;NkG0MlI2KG6P Mm\hV2FPT0WU
MOLT-16 NFrzVVRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEn5Z|FKSzVyPU[zNU4{OiCwTR?= M1Kw[3NCVkeHUh?=
GB-1 NYjO[49HT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF\afo5KSzVyPUexNE4zOyCwTR?= NXPnVWFJW0GQR1XS
TE-12 M4DJdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml7TTWM2OD16MESuOVUhdk1? NEn4W2JUSU6JRWK=
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LC-2-ad MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVezVVVJUUN3ME2xMlEyPDB5IN88US=> MmLhV2FPT0WU
BL-70 Mki1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NETlU5pKSzVyPUGuNVE5PDZizszN NHfwOFdUSU6JRWK=
ETK-1 NHTVPW5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mkf2TWM2OD1zLkK4OVgh|ryP MUPTRW5ITVJ?
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OCI-AML2 NYTSNVJyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3PjW2lEPTB;MT6zOlg2OSEQvF2= NEH4d4RUSU6JRWK=
SIG-M5 M3zwR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4LOdmlEPTB;MT6zO|AxQSEQvF2= NVrq[oZZW0GQR1XS
NCI-SNU-16 M{Dzcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3LX[WlEPTB;MT60OlQ5PiEQvF2= NEXKVJRUSU6JRWK=
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A3-KAW MlzXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1js[2lEPTB;MT62NlU1PiEQvF2= NF\pUYhUSU6JRWK=
KS-1 M4jGe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NULNSYkzUUN3ME2xMlY6OjR5IN88US=> MoPnV2FPT0WU
CTV-1 Ml;SS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkLZTWM2OD1zLkeyO|UyKM7:TR?= MVvTRW5ITVJ?
LB1047-RCC Mne2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mk\JTWM2OD1zLkixOlI1KM7:TR?= NEDVU2NUSU6JRWK=
EMG-01 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXjaS21pUUN3ME2xMlg{PTZ|IN88US=> MXjTRW5ITVJ?
TE-11 M2CyeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{TGeGlEPTB;MT64N|k5PSEQvF2= M3T5PXNCVkeHUh?=
CMK MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2Xie2lEPTB;MT65OVUyPyEQvF2= NVribGlXW0GQR1XS
NB1 NGDmZW9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVvMdmVmUUN3ME2xMlk3OTF5IN88US=> MlPrV2FPT0WU
HAL-01 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXTlVVBHUUN3ME2yMlA2QTR4IN88US=> M4\HOXNCVkeHUh?=
DEL M1;vd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1TZW2lEPTB;Mj6wPFQ5OiEQvF2= NYGxdItFW0GQR1XS
RL95-2 M1XJO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWDJR|UxRTJwMUGxN|ch|ryP NU[zT5N{W0GQR1XS
KARPAS-299 M13iN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlfyTWM2OD1{LkGxN|E{KM7:TR?= M4PkR3NCVkeHUh?=
EW-16 M4LoUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M33xZWlEPTB;Mj6xN|UxQCEQvF2= NYfqWZJmW0GQR1XS
RS4-11 MmWwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFHvZWxKSzVyPUKuNVc6OjRizszN NGPRN4hUSU6JRWK=
BB30-HNC NIXZS4FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVjJR|UxRTJwMkKzO|Uh|ryP MmruV2FPT0WU
DOHH-2 NV;jeZBjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIPHUFdKSzVyPUKuN|M1OzFizszN MmDWV2FPT0WU
RPMI-8402 MmP1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUTieVBKUUN3ME2yMlM{PjF6IN88US=> NH\NWoFUSU6JRWK=
BV-173 M1WwZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4jQPGlEPTB;Mj6zN|Y3KM7:TR?= NH61UoNUSU6JRWK=
TE-10 MnTWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoqyTWM2OD1{LkO0N|g1KM7:TR?= MXXTRW5ITVJ?
TE-8 M2e3[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUj5fHJxUUN3ME2yMlM4ODN6IN88US=> Moe5V2FPT0WU
K052 M4LuWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1\EdWlEPTB;Mj60NFIxOiEQvF2= M3nYdXNCVkeHUh?=
KARPAS-45 NVH1RopZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{LyVmlEPTB;Mj60PVQ1PiEQvF2= M4rUPXNCVkeHUh?=
SK-NEP-1 NWXVSJhUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlPGTWM2OD1{Lk[wNlM4KM7:TR?= NELvN|dUSU6JRWK=
KGN NW\nTlBzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWDJR|UxRTJwNkCzN|kh|ryP NUjTVlFFW0GQR1XS
ML-2 MnTYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWfJR|UxRTJwNkO1NVIh|ryP NYr5NphmW0GQR1XS
LAMA-84 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NInIUoRKSzVyPUKuOlk2PDVizszN M{LUOnNCVkeHUh?=
LXF-289 MnjXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2LrcmlEPTB;Mj63Nlk5QSEQvF2= NXL3U21XW0GQR1XS
A101D MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkjUTWM2OD1{Lke4N|A1KM7:TR?= MXLTRW5ITVJ?
KY821 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1\zbmlEPTB;Mj63PVc2QCEQvF2= NGnBZ2pUSU6JRWK=
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RPMI-6666 NI[2OFhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1\SZ2lEPTB;Mz61OFE4OSEQvF2= NXTuSolZW0GQR1XS
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JAR MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MW\JR|UxRTNwOUi4N|Ih|ryP MonGV2FPT0WU
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DU-4475 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{T6TWlEPTB;ND6zOlczQSEQvF2= MojNV2FPT0WU
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SW982 M17ofmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NY\TclVWUUN3ME20MlU2OzB5IN88US=> NX3WT4duW0GQR1XS
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SH-4 MlTxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mof5TWM2OD13LkS4N|ch|ryP MVLTRW5ITVJ?
MHH-CALL-2 MmPUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{PrfGlEPTB;NT63OlcyQSEQvF2= M2\QdnNCVkeHUh?=
KG-1 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4TGT2lEPTB;Nj6wNlg4QCEQvF2= MUnTRW5ITVJ?
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ST486 MoDYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3freGlEPTB;Nj6zOFcyKM7:TR?= M2HOZXNCVkeHUh?=
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KU812 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIrWOnpKSzVyPU[uOlk1OiEQvF2= NV7VbpFQW0GQR1XS
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NCI-H1355 NFTnfXNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3zuUGlEPTB;Nz60OVgxPCEQvF2= Mm[yV2FPT0WU
RPMI-8226 NH7HV49Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF\ieolKSzVyPUeuOVA4OzlizszN NV;FSGlHW0GQR1XS
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KARPAS-422 MoDkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2\OPGlEPTB;Nz61O|IxPiEQvF2= MVrTRW5ITVJ?
CA46 NGj0[JZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MY\JR|UxRTdwNUiwNVIh|ryP NFPERmJUSU6JRWK=
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no-11 MoPQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2XY[GlEPTB;Nz63O|U2PyEQvF2= MnrFV2FPT0WU
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NCI-H209 Mn33S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mo\GTWM2OD16LkGxOlUzKM7:TR?= NEXhV4tUSU6JRWK=
TALL-1 Ml;MS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUfJR|UxRThwMUizPFQh|ryP MkTpV2FPT0WU
KMOE-2 Mk\MS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NISyZ|lKSzVyPUiuNVk1OiEQvF2= NXXw[IhVW0GQR1XS
HCC1599 M1GzWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1mxTWlEPTB;OD6xPVk5PyEQvF2= NWHWUG94W0GQR1XS
CI-1 Ml7mS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUTJR|UxRThwMkC0NVEh|ryP NYi2[oRHW0GQR1XS
NCI-H1304 M37Ie2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUPJR|UxRThwMkC2OlEh|ryP M2n6fXNCVkeHUh?=
Daudi M1vu[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmLlTWM2OD16LkKzOVQ3KM7:TR?= MWLTRW5ITVJ?
CPC-N M2fWT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYLNRpE3UUN3ME24MlI6OTl7IN88US=> NFzaUm9USU6JRWK=
MC-CAR M2DxRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2T4ZWlEPTB;OD6zN|U5KM7:TR?= M2TXbnNCVkeHUh?=
SW872 NIHJUVNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVvxPYx5UUN3ME24MlM1PzV6IN88US=> M3HjXHNCVkeHUh?=
OVCAR-4 NW\rcphST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{PNRmlEPTB;OD61NFM2OSEQvF2= M3HuU3NCVkeHUh?=
OCUB-M MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mor3TWM2OD16LkW2OVA5KM7:TR?= M{fuRXNCVkeHUh?=
SK-PN-DW MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVrSRph1UUN3ME24MlYxQTh3IN88US=> M2LoPXNCVkeHUh?=
NCCIT NGCxSI1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIHQR4xKSzVyPUiuO|E4PDVizszN M4LZSXNCVkeHUh?=
NCI-H1648 M3fFV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFnqdJBKSzVyPUmuNVM5OzRizszN M{jNdnNCVkeHUh?=
COR-L279 NYrQbZh3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHXPd4dKSzVyPUmuN|kxQSEQvF2= MojuV2FPT0WU
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ONS-76 NEPhVoJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnrZTWM2OD17LkixNFE3KM7:TR?= M4HxPHNCVkeHUh?=
VA-ES-BJ M2nVU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NU\DToRKUUN3ME25Mlk6QTN|IN88US=> MkXqV2FPT0WU
GR-ST NUPnWoRoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVf3NFB1UUN3ME2xNE4zOjB5IN88US=> MVLTRW5ITVJ?
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RXF393 Mle4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIDHdnpKSzVyPUGxMlQ5OzRizszN M3j5OnNCVkeHUh?=
NCI-H2107 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoriTWM2OD1zMT61PVg1KM7:TR?= NYC2bYN1W0GQR1XS
K562 M2nZcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVfJR|UxRTFzLki3NFIh|ryP MXLTRW5ITVJ?
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COLO-320-HSR MoLUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M37YfmlEPTB;MUKuNVU3PSEQvF2= MlPxV2FPT0WU
K5 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1PGOWlEPTB;MUKuNlk5PSEQvF2= MmDUV2FPT0WU
BC-3 NF6zZ4xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH7UdlJKSzVyPUGyMlQ3PTFizszN MVPTRW5ITVJ?
REH MljNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVnNOI1PUUN3ME2xNk43PDl6IN88US=> Mn\wV2FPT0WU
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NCI-H128 M1vwRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4LPXGlEPTB;MUOuNFczOyEQvF2= M3PqW3NCVkeHUh?=
NCI-H1694 M3HRb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHrmd4xKSzVyPUGzMlEyPDRizszN MlrjV2FPT0WU
TGW NXL4OGtnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4H2cWlEPTB;MUOuN|I4PiEQvF2= MoTRV2FPT0WU
NCI-SNU-1 Mk\uS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXrFfVlMUUN3ME2xN{4{PDVizszN NXP4Nod5W0GQR1XS
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CTB-1 MnP4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnXXTWM2OD1zMz63Nlk1KM7:TR?= MV\TRW5ITVJ?
HUTU-80 MlzOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYfJR|UxRTF|Lke1O|Mh|ryP NVnMcFlyW0GQR1XS
LAN-6 M2r5Umdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3LiU2lEPTB;MUSuNlQ2PyEQvF2= M4raNXNCVkeHUh?=
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NCI-H1770 NYHtSGNNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3jUR2lEPTB;MUSuOVM3QSEQvF2= NG\xOG1USU6JRWK=
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COR-L88 MkK4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mof3TWM2OD1zNj6wNFEzKM7:TR?= NVLuUnRmW0GQR1XS
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D-283MED Mmn4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWDZeol{UUN3ME2xOk45PDh7IN88US=> M{XFbXNCVkeHUh?=
NCI-H719 NUPVdopCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoHCTWM2OD1zNj65NVYyKM7:TR?= NGq1bmxUSU6JRWK=
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SK-N-FI MlnwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2jQc2lEPTB;MUeuOlkyOyEQvF2= MY\TRW5ITVJ?
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NCI-H1882 M{fi[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF7wdldKSzVyPUG3Mlk5OzRizszN NYGxVII2W0GQR1XS
A704 NVHRSHlQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGLqcVNKSzVyPUG3Mlk6ODRizszN NFj6XW1USU6JRWK=
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HCC1187 M3XZbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX[ybXFjUUN3ME2xPE4xOTh5IN88US=> NV:wOpFVW0GQR1XS
NCI-H1581 M2C1Vmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmnPTWM2OD1zOD6wPFY3KM7:TR?= NHnTfY9USU6JRWK=
BB65-RCC MmTtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUfzfZdRUUN3ME2xPE41OTZ{IN88US=> M{jxNHNCVkeHUh?=
EM-2 NWTUVmxZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFe1VJVKSzVyPUG4MlU3PzJizszN MXLTRW5ITVJ?
Raji NUHmc4puT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoTWTWM2OD1zOT65OVY2KM7:TR?= NXLreItlW0GQR1XS
TE-1 NYi4UopUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NETiNlhKSzVyPUKwMlQyODRizszN NUnRc254W0GQR1XS
SW962 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{jWdGlEPTB;MkCuOFI6OyEQvF2= M3m2XXNCVkeHUh?=
MHH-NB-11 NGK0VmdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYLJR|UxRTJyLkW1NlEh|ryP Mn74V2FPT0WU
no-10 MniwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MW\JR|UxRTJzLkCyOlQh|ryP NXvQb5ZrW0GQR1XS
GDM-1 NH7je4xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NETlWGxKSzVyPUKxMlk1OTRizszN M2\lc3NCVkeHUh?=
KMS-12-PE MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MULJR|UxRTJ{LkK3OEDPxE1? NWO5Wm9TW0GQR1XS
NCI-H510A M37iZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlrzTWM2OD1{ND6xNlc5KM7:TR?= MXLTRW5ITVJ?
ES5 M1rxcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2DmRWlEPTB;MkSuO|M1QSEQvF2= MV7TRW5ITVJ?
JiyoyeP-2003 M3HvXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M17RWmlEPTB;Mk[uNlc1OiEQvF2= NHSwU4tUSU6JRWK=
NMC-G1 NWX2WlZsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUj2PJI4UUN3ME2yO{4yQDJ{IN88US=> MmLxV2FPT0WU
NCI-H446 M1zvTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MU\JR|UxRTJ5LkS5OFYh|ryP NELKXnVUSU6JRWK=
NB7 NEjy[ldIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoXxTWM2OD1{Nz65NlI6KM7:TR?= Ml\MV2FPT0WU
A388 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGXYfINKSzVyPUK4MlAxPzRizszN Mm[4V2FPT0WU
JVM-2 NX;NeVBET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{PkfGlEPTB;MkiuNlg6QCEQvF2= MXzTRW5ITVJ?
HT-144 NWju[|hST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWD3epk{UUN3ME2yPE43QSEQvF2= Mom5V2FPT0WU
NCI-H747 M4Txcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYHJR|UxRTJ6LkmxPVUh|ryP MWHTRW5ITVJ?
NCI-H1650 M4PuUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIHCZ5pKSzVyPUK5MlAyPzZizszN NFPqNVFUSU6JRWK=
EB-3 MmWxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYrBSpFFUUN3ME2yPU42OzB7IN88US=> NF\PepZUSU6JRWK=
KLE NHHjXJhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUfwXpV7UUN3ME2yPU43OTlizszN MmXZV2FPT0WU
TK10 M3vob2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXrKSIlXUUN3ME2zNE4yOjZizszN Mm\DV2FPT0WU
COLO-668 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYm1RZdbUUN3ME2zNE44QTJizszN MWHTRW5ITVJ?
NCI-H23 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3P6PGlEPTB;M{GuNVA3OyEQvF2= NH\pTlZUSU6JRWK=
GOTO MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NE\KO|NKSzVyPUOxMlYxQDVizszN MWHTRW5ITVJ?
MSTO-211H NYHyOYY3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWXJR|UxRTNzLki2O|gh|ryP Mnv1V2FPT0WU
LB831-BLC NGjqN4hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXLJR|UxRTN{LkO4OFMh|ryP MW\TRW5ITVJ?
SCH Moe5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGjUb4xKSzVyPUOyMlg1QDVizszN MnXVV2FPT0WU
EHEB MkixS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYjHUHlIUUN3ME2zOE4yOTl|IN88US=> NFPKdXhUSU6JRWK=
U-266 Mn7rS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn;LTWM2OD1|ND6yO|gyKM7:TR?= MUjTRW5ITVJ?
EW-11 NVfYWHp7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWf3bZd[UUN3ME2zOE41PzJ3IN88US=> MkSxV2FPT0WU
TE-9 M4XUO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlXlTWM2OD1|Nz6wOFAyKM7:TR?= MVnTRW5ITVJ?
ES3 Mn3vS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlHaTWM2OD1|Nz61NFA1KM7:TR?= NFX3bJlUSU6JRWK=
NCI-H2141 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYDJR|UxRTN6LkC4OFMh|ryP M3ix[3NCVkeHUh?=
MPP-89 M1XpV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEXDfIJKSzVyPUSyMlA2QDZizszN M3TDfnNCVkeHUh?=
SK-MEL-2 NXvXV25KT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3HlU2lEPTB;NEKuOlQxPSEQvF2= NVn2U3RrW0GQR1XS
LC-1F NIixOW5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXnJR|UxRTR|LkO2PFIh|ryP M4XyNHNCVkeHUh?=
NH-12 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYHJR|UxRTR|LkmzOVkh|ryP NHPDTGVUSU6JRWK=
RKO NGW2UWVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWjOOHpLUUN3ME20OE4yOjV{IN88US=> NELpeFRUSU6JRWK=
KM-H2 NU\zVFhNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGHabGtKSzVyPUS0Mlk2PzdizszN NGH1dVRUSU6JRWK=
SK-UT-1 NF\1OJdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVfrOHRuUUN3ME20PU45QDJ3IN88US=> MoXOV2FPT0WU

... Click to View More Cell Line Experimental Data

In vivo Consistent with the substantial and selective inhibition of VEGFR2 or PDGFR phosphorylation and signaling in vivo, Sunitinib (20-80 mg/kg/day) exhibits broad and potent dose-dependent anti-tumor activity against a variety of tumor xenograft models including HT-29, A431, Colo205, H-460, SF763T, C6, A375, or MDA-MB-435. Sunitinib dosing at 80 mg/kg/day for 21 days leads to complete tumor regression in six of eight mice, without tumor re-growing during a 110-day observation period after the end of treatment. Second round of treatment with Sunitinib remains efficacious against tumors that are not fully regressed during the first round of treatment. Sunitinib treatment results in significant decrease in tumor MVD, with ~40% reduction in SF763T glioma tumors. SU11248 treatment results in a complete inhibition of additional tumor growth of luciferase-expressing PC-3M xenografts, despite no reduction in tumor size. [2] Sunitinib treatment (20 mg/kg/day) dramatically suppresses the growth subcutaneous MV4;11 (FLT3-ITD) xenografts and prolongs survival in the FLT3-ITD bone marrow engraftment model. [3]

Protocol

Kinase Assay:[1]
+ Expand

Biochemical Tyrosine Kinase Assays:

IC50 values for Sunitinib against VEGFR2 (Flk-1) and PDGFRβ are determined using glutathione S-transferasefusion proteins containing the complete cytoplasmic domain of the RTK. Biochemical tyrosine kinase assays to quantitate the trans-phosphorylation activity of VEGFR2 (Flk-1) and PDGFRβ are performed in 96-well microtiter plates precoated (20 μg/well in PBS; incubated overnight at 4 °C) with the peptide substrate poly-Glu,Tyr (4:1). Excess protein binding sites are blocked with the addition of 1-5% (w/v) BSA in PBS. Purified GST-fusion proteins are produced in baculovirus-infected insect cells. GST-VEGFR2 and GST-PDGFRβ are then added to the microtiter wells in 2 × concentration kinase dilution buffer consisting of 100 mM HEPES, 50 mM NaCl, 40 μM NaVO4, and 0.02% (w/v) BSA. The final enzyme concentration for GST-VEGFR2 or GST-PDGFRβ is 50 ng/mL. Twenty-five μL of diluted Sunitinib are subsequently added to each reaction well to produce a range of inhibitor concentrations appropriate for each enzyme. The kinase reaction is initiated by the addition of different concentrations of ATP in a solution of MnCl2 so that the final ATP concentrations spanned the Km for the enzyme, and the final concentration of MnCl2 is 10 mM. The plates are incubated for 5-15 minutes at room temperature before stopping the reaction with the addition of EDTA. The plates are then washed three times with TBST. Rabbit polyclonal antiphosphotyrosine antisera are added to the wells at a 1:10,000 dilution in TBST containing 0.5% (w/v) BSA, 0.025% (w/v) nonfat dry milk, and 100 μM NaVO4 and incubated for 1 hour at 37 °C. The plates are then washed three times with TBST, followed by the addition of goat antirabbit antisera conjugated with horseradish peroxidase (1:10,000 dilution in TBST). The plates are incubated for 1 hour at 37 °C and then washed three times with TBST. The amount of phosphotyrosine in each well is quantitated after the addition of 2,2′-azino-di-[3-ethylbenzthiazoline sulfonate] as substrate.
Cell Research:[3]
+ Expand
  • Cell lines: RS4;11, MV4;11, and OC1-AML5
  • Concentrations: Dissolved in DMSO, final concentrations ~10 μM
  • Incubation Time: 24 and 48 hours
  • Method: Cells are starved overnight in medium containing 0.1% FBS prior to addition of Sunitinib and FL (50 ng/mL; FLT3-WT cells only). Proliferation is measured after 48 hours of culture using the Alamar Blue assay or trypan blue cell viability assays. Apoptosis is measured 24 hours after Sunitinib addition by Western blotting to detect cleavage of poly (ADP-ribose) polymerase (PARP) or levels of caspase-3.
    (Only for Reference)
Animal Research:[2]
+ Expand
  • Animal Models: Female nu/nu mice implanted s.c. with HT-29, A431, Colo205, H-460, SF763T, C6, A375, or MDA-MB-435, and male nu/nu mice bearing luciferase-expressing PC-3M tumors
  • Formulation: Formulated as a carboxymethyl cellulose suspension or as a citrate buffered (pH 3.5) solution
  • Dosages: ~80 mg/kg
  • Administration: Orally once daily
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 15 mg/mL (28.16 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents individually and in order:
4% DMSO+30% PEG 300+ddH2O
2mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 532.56
Formula

C22H27FN4O2.C4H6O5

CAS No. 341031-54-7
Storage powder
Synonyms N/A

Bio Calculators

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Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

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Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02761057 Recruiting Recurrent Renal Cell Carcinoma|Stage III Renal Cell Cancer|Stage IV Renal Cell Cancer|Type 1 Papillary Renal Cell Carcinoma|Type 2 Papillary Renal Cell Carcinoma National Cancer Institute (NCI) April 2016 Phase 2
NCT02779283 Recruiting Untreated Adult Acute Myeloid Leukemia OHSU Knight Cancer Institute|National Cancer Institute (NCI) December 2015 Phase 1
NCT02626754 Enrolling by invitation Renal Cell Carcinoma vghtpe user|Taipei Veterans General Hospital, Taiwan August 2015 Phase 2
NCT02465060 Recruiting Advanced Malignant Neoplasm|Lymphoma|Recurrent Plasma Cell Myeloma|Recurrent Solid Neoplasm|Refractory Malignant Neoplasm|Refractory Plasma Cell Myeloma National Cancer Institute (NCI) August 2015 Phase 2
NCT01835158 Active, not recruiting Clear Cell Renal Cell Carcinoma|Metastatic Renal Cell Cancer|Stage III Renal Cell Cancer|Stage IV Renal Cell Cancer National Cancer Institute (NCI) July 2013 Phase 2
NCT01740154 Terminated Fatigue|Recurrent Renal Cell Cancer|Stage IV Renal Cell Cancer Case Comprehensive Cancer Center|National Cancer Institute (NCI) September 2012 --

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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Frequently Asked Questions

  • Question 1:

    I was wondering that the compound is in its cis or trans form?

  • Answer:

    S1042 Sunitinib Malate is Z form.

  • Question 2:

    What is the difference between Sunitinib Malate(S1042) and Sunitinib(S7781)?

  • Answer:

    S1042 is the Malate salt form of Sunitinib. The biological activities of these two compounds are the same but the solubility of these two compounds in aqueous solvent are different.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID